期刊
INTERNATIONAL JOURNAL OF PHARMACEUTICS
卷 202, 期 1-2, 页码 173-178出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/S0378-5173(00)00426-9
关键词
hydroxypropylmethylcellulose; macrogol 6000; sustained release tablet; nifedipine
The aim of the present study was to investigate the effect of hydroxypropylmethylcellulose (HPMC-2208), used as an excipient for controlled release of drug, on the release profiles and bioavailability of the poorly water-soluble nifedipine (NP) from a tablet prepared using macrogol 6000 (PEG) and HPMC. The crushing tolerance of the NP tablet prepared using PEG and HPMC (NP-PEG-HPMC tablet) was markedly increased with increasing compression force used during the preparation from 20 to 200 MPa. The values reached their maximal levels (approximately 13 kg for the NP-PEG-HPMC tablet and 8 kg for the PEG tablet) at the compression force of 100 MPa. Although NP is a poorly water-soluble drug, it was rapidly dissolved from the NP-PEG tablet (without HPMC) due to the improvement of its dissolution rate in the presence of PEG. NP dissolution was complete at the latest within 1 h. On the other hand, dissolution of NP from the NP-PEG-HPMC tablet was significantly delayed with an increase in the concentration of HPMC in the tablet. The dissolution of NP from the NP-PEG-HPMC tablet containing 50% HPMC-2208 was markedly delayed as the viscosity of HPMC also increased. Interestingly, the same peak plasma NP concentration (C-max) and the area under the plasma NP concentration-time curve (AUC(0) (10)) were observed for both the NP-PEG tablet and NP-PEG-HPMC tablets, however, the time to C-max (t(max)) for the NP-PEG-HPMC tablet was significantly higher when the NP-PEG-HPMC tablet using a mixture of NP-PEG granules (prepared with PEG) and HPMC. (C) 2000 Elsevier Science B.V. All rights reserved.
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